美国FDA日前批准使用Xifaxan（利福昔明）减少在老年肝病患者因反复细菌性痢疾中导致的肝性脑病风险。这种药品被批准在旅行者腹泻中使用，这是利福昔明的新用法。 肝性脑病是一种已经失去清除毒素肝脏的患者恶化的脑功能障碍，不断上升的血氨水平在肝性脑病的发展中有重要的作用，而利福昔明的作用就是减低血氨的水平。 利福昔明的作用在美国、加拿大、俄罗斯的一项与安慰剂的对照临床试验中得到了证实，进入次试验的肝病患者没有或者是肝性脑病的症状很轻，与安慰剂相比，服用利福昔明的患者的肝性脑病很少发生。大部分使用利福昔明的肝病患者的共同的副作用是上、下肢的水肿（周围水肿）、恶心、胀气和头痛。 部分中文Xifaxan处方资料（仅供参考） 英文药名: 利福昔明片Xifaxan(Rifaximin Tablets) 中文药名: 利福昔明片 药品名称 通用名：利福昔明片 英文名：Rifaximin Tablets 成分：利福昔明。 化学名称：4-脱氧-4-甲基砒啶[1，2-1，2]咪唑井[5，4-环]利福霉素SV。 分子式：C13H51N13O11 分子量：785.89 药品介绍 美国食品药品管理局于2010年3月24日宣布，它已批准将Xifaxan(利福昔明) 用于晚期肝病患者，作为降低其显性肝性脑病(HE)复发风险的一种手段。Xifaxan之前曾被批准用于治疗旅行者腹泻。 一项随机安慰剂对照临床证实了Xifaxan用于预防HE的有效性，该试验的受试者由来自美国、加拿大和俄罗斯的成年肝病患者组成。Xifaxan在最严重肝病患者中的疗效未被研究。试验受试者从未或仅出现过轻微的HE症状。与接受安慰剂对照的受试者相比，接受Xifaxan治疗的患者在试验期间更少出现HE。然而，由于大部分患者在试验期间同时还在服用乳果糖，所以尚无法评估Xifaxan作为HE的一种独立疗法的疗效。 使用Xifaxan治疗肝病患者所报告的最常见不良反应包括外周性水肿、恶心、打嗝及头痛。 Salix公司表示美国FDA专家顾问委员会表示支持利福昔明（rifaximin，Xifaxan）550 mg片剂用于治疗慢性肝衰竭引起的神经系统损害，顾问委员会投过投票表示支持该药用于肝性脑病。肝衰竭患者的肝性脑病引起神经损害，导致患者出现昏迷与无意识症状。 本品已获得了用于此症的罕用药地位，将在美国获得7年的市场独占权。在Ⅲ期临床研究中，本品显著降低肝性脑病复发风险。肝性脑病常发生在肝硬化患者中，在美国有60万肝硬化患者。本品现在以商品名Xifaxan在美国销售用于由埃希氏菌属引起的旅行者腹泻。 药理作用 药理作用：利福昔明是广谱肠道抗生素。它是利福霉素SV的半合成衍生物。利福昔明和其它利福霉素类抗生素一样，通过与细菌DNA-依赖RNA聚合酶的B-亚单位不可逆转地结合而抑制细菌RNA的合成，最终抑制细菌蛋白质的合成。由于其与酶的结合是不可逆的，所以其活性为对敏感菌的杀菌活性。对利福昔明抗菌活性的研究资料显示，本品与利福霉素具有同样广泛的抗菌谱，对多数革兰氏阳性菌和革兰氏阴性菌，包括需氧菌和厌氧菌的感染具有杀菌作用。由于利福昔明口服时不被胃肠道吸收，所以它是通过杀灭肠道的病原体而在局部发挥抗菌作用。毒理作用：重复给药毒性：大鼠每天口服本品25,50及100mg/kg，连续180天后，耐受性好，除雌鼠血清总胆固醇呈剂量相关性增加外(可能为对肠道菌群产生作用的结果)，未见其他异常改变。遗传毒性：体内外研究未见本品有致突变作用。生殖毒性：大鼠及家兔给予本品50及100mg/kg未见致畸作用及其他生殖毒性。 药代动力学 在鼠，家狗和人体药代动力学的研究证明，本品经口服不被吸收(吸收小于1%)。 适应症 对利福昔明敏感的病原菌引起的肠道感染，包括急性和慢性肠道感染，腹泻综合症，夏季腹泻，旅行者腹泻和小肠结肠炎等。 用法用量 成人口服。每次0.2g(1片)，每日3-4次。 6-12岁儿童口服。每次0.1-0.2g(0.5-1片)，每日4次。 12岁以上儿童，剂量同成人。 可根据医嘱调节剂量和服用次数。除非是遵照医嘱的情况下，每一疗程不应超过7天。 不良反应 部分患者用药后可出现恶心（通常出现在第一次服药后），但症状可迅速消退。大剂量长期用药，极少数患者可能出现蕈麻疹样皮肤反应。 1，中枢神经系统有出现头痛的报道。 2，代谢/分泌系统肝性脑病患者服用本药后可出现体重下降，血清钾和血清钠浓度轻度升高。 3，胃肠道系统常见的症状为腹涨，腹痛，恶心和呕吐。以上症状发生率者均低于1%。 4，皮肤大剂量长期用药，极少数患者可能出现蕈麻疹样皮肤反应。 5，其他有用药后可能引起足水肿的报道。 禁忌 以下患者禁用： 1.对本药或利福霉素过敏者； 2.肠梗阻者； 3.严重的肠道溃疡性病变者。 注意事项 1.儿童连续服用本药不能超过7日。 2.对6岁以下儿童建议不要服用本药片剂。 3.长期大剂量用药或肠黏膜受损时，会有极少量（少于1%）被吸收，导致尿液呈粉红色。 4.请置于儿童触及不到的地方。 5.如果出现对抗生素不敏赶的微生物，应中断治疗并采取其他适当治疗措施。 6.对驾驶和操纵机器的影响，未知。 孕妇及哺乳期妇女用药 1.药物对妊娠的影响：动物实验本药无致畸作用。但妊娠期妇女用药的安全性和有效性尚不明确。因此，妊娠期妇女需权衡利弊后用药。 2.药物对哺乳的影响：本药口服后只有极少量被吸收，在乳汁中的浓度也极低，哺乳期妇女可在有适当医疗监测的情况下服用本药。 儿童用药[] 建议6岁以下儿童不要服用，6岁及6岁以上儿童服用方法请参见[用法用量]。 药物相互作用 口服利福昔明只有少于1%口服剂量经胃肠道吸收，所以利福昔明不会引起因药物的相互作用而导致的全身问题。 药物过量 试验证明服用本品剂量达1.6g/日，既没有局部也没有全身的不良事件发生。一旦过量服用应洗胃，并配合其他适当治疗。 XIFAXAN 550mg Generic Name for XIFAXAN 550mg Rifaximin 550mg; tabs. Legal Classification: Rx Pharmacological Class for XIFAXAN 550mg Rifamycin. Manufacturer of XIFAXAN 550mg Salix Pharmaceuticals, Inc. Indications for XIFAXAN 550mg Reduction in risk of overt hepatic encephalopathy recurrence in patients ≥18yrs of age. Adult dose for XIFAXAN 550mg ≥18yrs: 550mg twice daily. Children's dosing for XIFAXAN 550mg <18yrs: not recommended. Warnings/Precautions for XIFAXAN 550mg Not studied in patients with MELD scores >25; only 8.6% of patients in the controlled trial had MELD >19. Increased systemic exposure in patients with more severe hepatic dysfunction; caution should be exercised in patients with severe hepatic impairment (Child-Pugh C). Elderly. Pregnancy (Cat.C). Nursing mothers: not recommended. Adverse Reactions for XIFAXAN 550mg Peripheral edema, nausea, dizziness, fatigue, ascites. How is XIFAXAN 550mg supplied? Tabs—60 注：以下产品不同规格和不同价格，购买时请以电话咨询为准！ --------------------------------------------------------------- 原产地英文商品名: XIFAXAN UNIT DOSE PACK 550mg/tab 60tabs/bottle 原产地英文药品名: RIFAXIMIN 中文参考商品译名: XIFAXAN单位剂量包装 550毫克/片 60片/瓶 中文参考药品译名: 利福昔明 中文参考化合物名称: 4-脱氧-4-甲基砒啶[1，2-1，2]咪唑井[5，4-环]利福霉素SV 生产厂家中文参考译名: SALIX PHARMS 生产厂家英文名: SALIX PHARMS --------------------------------------------------------------- 原产地英文商品名: XIFAXAN UNIT DOSE PACK 200mg/tab 100tabs/bottle 原产地英文药品名: RIFAXIMIN 中文参考商品译名: XIFAXAN单位剂量包装 200毫克/片 100片/瓶 中文参考药品译名: 利福昔明 中文参考化合物名称: 4-脱氧-4-甲基砒啶[1，2-1，2]咪唑井[5，4-环]利福霉素SV 生产厂家中文参考译名: SALIX PHARMS 生产厂家英文名: SALIX PHARMS   --------------------------------------------------------------- Welcome to Xifaxan550.com Xifaxan (rifaximin) 550 mg is an antibiotic that can help reduce the risk of overt hepatic encephalopathy (HE) recurrence in adults. Whether you are a patient or caregiver, this Web site is designed to help you learn more about Xifaxan 550 mg, overt hepatic encephalopathy, and support options, like H.E.L.P.—the HE Living Program. Explore this site to learn about Xifaxan 550 mg and how it can: Lower your risk of overt HE recurrence Reduce your chances of being hospitalized because of HE Learn how Xifaxan 550 mg can help reduce the risk of overt HE recurrence Learn more about HE    IMPORTANT SAFETY INFORMATION XIFAXAN (rifaximin) 550 mg tablets are approved to reduce the risk of overt hepatic encephalopathy (HE) recurrence in people 18 and older. In a scientific study of XIFAXAN for HE, 91% of patients were also taking lactulose. XIFAXAN has not been studied in people with MELD scores >25, and only 8.6% of people in the controlled study had MELD scores over 19. There is an increased chance that XIFAXAN will spread through your body if you have more severe hepatic dysfunction. Therefore, if you have severe hepatic impairment, which is a Child-Pugh score of C, you should exercise caution when taking XIFAXAN. XIFAXAN is not for everyone. Do not take XIFAXAN if you have a known hypersensitivity to rifaximin or any of the components in XIFAXAN. XIFAXAN, like nearly all antibiotics, can alter the normal flora of the colon. This can lead to an overgrowth of Clostridium difficile (C. difficile) bacteria. If you take XIFAXAN, there is a chance you could experience diarrhea caused by C. difficile. C. difficile can cause symptoms ranging in severity from mild diarrhea to life-threatening inflammation of the colon. If you suspect you have C. difficile–associated diarrhea, contact your healthcare provider immediately, as treatment may need to be discontinued. The most common side effects associated with XIFAXAN—occurring in more than 8% of people—were edema peripheral, nausea, dizziness, fatigue, ascites, muscle spasms, pruritus, and abdominal pain. You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch, or call 1-800-FDA-1088. Xifaxan550 is not available for sale outside the U.S. Xifaxan550 is licensed by Alfa Wassermann S.p.A. to Salix Pharmaceuticals, Inc. Complete Prescribing Information For product information, adverse event reports, and product complaint reports, please contact: Salix Product Information Call Center ----------------------------------------------------------------------------- XIFAXAN 200 mg is indicated for the treatment of travelers’ diarrhea caused by noninvasive strains of Escherichia coli in patients 12 years of age and older. Escherichia coli is the most common cause of travelers’ diarrhea in Latin America, the Caribbean, and Africa.3 XIFAXAN 200 mg, a minimally absorbed enteric antibiotic, targets pathogenic E coli without causing long-term changes to gut flora balance. XIFAXAN 200 mg is proven to treat travelers’ diarrhea, stopping symptoms in 79.2% of patients.* View complete Prescribing Information Important Safety Information about XIFAXAN 550 mg XIFAXAN® 550 mg is indicated for reduction in risk of overt hepatic encephalopathy (HE) recurrence in patients ≥18 years of age. In the trials of XIFAXAN for HE, 91% of the patients were using lactulose concomitantly. XIFAXAN has not been studied in patients with MELD scores >25, and only 8.6% of patients in the controlled trial had MELD scores over 19. There is increased systemic exposure in patients with more severe hepatic dysfunction. Therefore, caution should be exercised when administering XIFAXAN to patients with severe hepatic impairment (Child-Pugh C). XIFAXAN is contraindicated in patients with a hypersensitivity to rifaximin, any of the rifamycin antimicrobial agents, or any of the components in XIFAXAN. Hypersensitivity reactions have included exfoliative dermatitis, angioneurotic edema, and anaphylaxis. Clostridium difficile–associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including XIFAXAN, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon which may lead to overgrowth of C difficile. If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C difficile may need to be discontinued. The most common adverse reactions occurring in >8% of patients in the clinical study were edema peripheral (15%), nausea (14%), dizziness (13%), fatigue (12%), ascites (11%), muscle spasms (9%), pruritus (9%), and abdominal pain (9%). For complete Prescribing Information. Important Safety Information about XIFAXAN 200 mg XIFAXAN® (rifaximin) 200 mg Tablets are indicated for the treatment of patients (≥12 years of age) with travelers’ diarrhea caused by noninvasive strains of Escherichia coli. XIFAXAN should not be used in patients with diarrhea complicated by fever or blood in the stool or diarrhea due to pathogens other than E coli. XIFAXAN should be discontinued if diarrhea symptoms get worse or persist more than 24 to 48 hours and alternative antibiotic therapy should be considered. E coli has been shown to develop resistance to rifaximin in vitro. However, the clinical significance of such an effect has not been studied. In clinical trials, XIFAXAN was generally well tolerated. The most common side effects (vs placebo) were flatulence 11.3% (vs 19.7%), headache 9.7% (vs 9.2%), abdominal pain 7.2% (vs 10.1%), rectal tenesmus 7.2% (vs 8.8%), defecation urgency 5.9% (vs 9.2%), and nausea 5.3% (vs 8.3%). For complete Prescribing Information. *In a randomized, double-blind, placebo-controlled study conducted in Mexico, Guatemala, and Kenya, the efficacy of XIFAXAN 200 mg (orally 3 times a day for 3 days) was evaluated in 254 adult subjects with travelers' diarrhea. Stool specimens were collected before treatment and 1 to 3 days following the end of treatment to identify enteric pathogens, predominantly E coli. The clinical efficacy of XIFAXAN 200 mg was assessed by the time to return to normal, formed stools and resolution of symptoms. References: 1. Merck Manual Home Edition. http://www.merck.com/mmhe/index.html. Accessed January 7, 2010. 2. XIFAXAN [prescribing information]. Morrisville, NC: Salix Pharmaceuticals, Inc; 2010. 3. Yates J. Traveler’s diarrhea. Am Fam Physician. 2005;71:2095-2100. The information contained on this page is intended for US residents, healthcare providers, and pharmacists only. You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch, or call 1-800-FDA-1088. For product information, adverse event reports, and product complaint reports please call: Salix Product Information Call Center FDA批准利福昔明（Xifaxan）治疗肝性脑病新适应症 利福昔明(Rifaximin)为利福霉素的衍生物，通过与细菌DNA-依赖RNA聚合酶的β-亚单位不可逆的结合而抑制细菌RNA的合成，最终抑制细菌蛋白质的合成。是第一个非氨基糖苷类肠道用抗生素。临床主要用于对利福昔明敏感的病原菌引起的肠道感染。 2010年3月25日，美国食品药品管理局（FDA）宣布批准利福昔明（Xifaxan）用于降低肝性脑病（HE）的复发风险。此前Xifaxan曾作为治疗旅行者腹泻药物获批。此次利福昔明作为罕见病药获优先审评的资格并批准此新适应症。 一项安慰剂随机对照临床试验评估了Xifaxan治疗HE的有效性，该临床试验的受试者由美国、加拿大和俄罗斯的成年患者组成。参加试验的肝病患者为无HE症状或有轻度HE症状者，与使用安慰剂治疗的患者相比，使用Xifaxan治疗的患者更少出现肝性脑病。 Xifaxan在严重肝病患者中的疗效尚未得以确认。在试验过程中，由于大部分患者同时服用了半乳糖甙果糖（一种合成糖，有助于阻止肠道的氨吸收进入血液），因此，无法评估Xifaxan作为单独治疗HE的确切疗效。 Xifaxan的常见不良反应主要为上下肢肿胀（外周性水肿）、恶心、嗳气和头痛。 Xifaxan(利福昔明)用于肠易激综合症获优先审评 Salix Pharmaceuticals公司表示美国FDA已接受了Xifaxan(利福昔明)用于肠易激综合症的新药上市申请，并且给予了优先审评地位，所申报的规格为550mg的片剂。在Xifaxan用于肠易激综合症的3期试验中，表明该药可显著改善肠易激综合症的腹疼与腹胀。 公司表示很高兴FDA接受了上市申请并给予了优先审评地位，这表示该药有潜力给肠易激综合症患者带来显著的益处。Xifaxan(利福昔明)目前在美国已批准用于治疗旅行者腹泻与降低肝性脑病的复发风险。